萘普生微乳的制备及其对小鼠的抗炎镇痛作用  

Preparation and Anti-inflammatory and Analgesic Effects on Mice of Naproxen Microemulsions

作　　者：庄雪梅[1] 缑灵山[1] 孙凌燕[1] 田霞[1] 刘毅[1] 

机构地区：[1]徐州医学院药学院,江苏徐州221002

出　　处：《中国医药工业杂志》2011年第10期760-765,共6页Chinese Journal of Pharmaceuticals

基　　金：江苏省自然科学基金(BK2009523);江苏省高校科研成果产业化推进项目(JHZD09-23);江苏省高校自然科学基金(09KJB350003);江苏省高校省级重点实验室开放课题(JSBL0803;C0903;C0904);江苏省2010年度"青蓝工程"培养对象项目和本院研究生创新计划(2010YKYCX005)资助

摘　　要：利用伪三元相图,得到空白微乳的优化处方为Cremophor EL-中链甘油三酸酯-聚乙二醇400-注射用水(3.0:1.5:3.0:12.5,w/w)。在此基础上制备的o/w型萘普生微乳外观澄清,平均粒径为(52.5±3 2)nm,载药量为1.02%。进一步考察了萘普生微乳对小鼠的抗炎镇痛效果及其连续给药后对大鼠胃黏膜组织形态学的改变。结果表明,萘普生微乳中(60mg/kg)、高(120mg/kg)剂量组与阳性对照(阿司匹林肠溶片,100mg/kg)组和荼普生片剂(120mg/kg)组相比,具有相近或更强的抗炎镇痛作用,且微乳能减轻萘普生对大鼠胃黏膜的损伤作用。The optimized formulation of blank microemulsions selected by pseudo-ternary phase diagrams consisted of Cremophor EL-medium chain triglycerides-polyethylene glycol 400-water for injection at weight ratio of 3.0 ： 1.5 ： 3.0 ： 12.5. The oil-in-water microemulsions of naproxen were prepared based on the above formulation. The product was transparent and clear with the mean diameter of （52.5±3.2）nm and drug loading of 1.02 %. The anti-inflammatory and analgesic effects on mice as well as histomorphological changes in gastric mucosa of rats after continuous oral administration were further evaluated. Compared with the positive group （aspirin entric-coated tablets, 100 mg/kg） and naproxen tablets group （120 mg/kg）, the middle and high dose of naproxen microemulsions groups （60 and 120 mg/kg） demonstrated similar or more efficacious anti-inflammatory and analgesic effects on mice. In addition, the microemulsions could reduce the injury of gastric mucosa of rats induced by naproxen.

关 键 词：伪三元相图 萘普生微乳 抗炎 镇痛 制备 

分 类 号：R944.9[医药卫生—药剂学]